Fibroblast activation protein (FAP) is a serine protein that is selectively expressed in pathologic sites in the adults making it a target specific site for many therapeutic agents. Fibroblast activation protein (FAP) is expressed during tissue remodeling stage in embryonic development. However, in adults, fibroblast activation protein (FAP) is expressed in specific sites like cancer, arthritis, inflammation, injury, pulmonary fibrosis, etc. Fibroblast activation protein is widely believed to be expressed on stromal fibroblasts of epithelial cancer cells and promotes cancer cell growth and metastasis. The specificity of fibroblast activation protein offers potential to represent as a new drug target in the diagnosis and treatment of cancer. Various clinical trials are being conducted to assess the potential of treating cancer by inhibiting the fibroblast activation protein. Cancer cells are often very sensitive to growth factors. Development of cancer growth impeders such as fibroblast activation protein (FAP) inhibitors can provide promising results in cancer management.

Fibroblast activation protein (FAP) have similar specificity as dipeptidyl peptidases (DPPs) and prolyl oligopeptidase (PREP) which are also known to elevate in cancers. This leads to the need of development of inhibitors that are specific to fibroblast activation protein (FAP).

Huge opportunities lie in development of fibroblast activation protein (FAP) specific inhibitors. Vigorous research and development programs are being conducted for the development of such inhibitors. One such inhibitor is Val-boroPro (Talabostat) which is a single-agent inhibitor of fibroblast activation protein (FAP) enzymatic activity. A number of clinical trials have been conducted to assess the efficacy of talabostat as fibroblast activation protein (FAP) inhibitor in different cancers such as colorectal, lung, pancreatic, leukemia and melanoma. Another approach being used in developing fibroblast activation protein (FAP) inhibitor is monoclonal antibodies. However, such approaches have not been extensively used in the clinical setting, mainly due to absence of effective actions.

Due to the rise in the prevalence of cancer globally, fibroblast activation protein (FAP) inhibitors are anticipated to assist in prevention of proliferation of these carcinogenic cells. According to the National Cancer Institute, an estimated 1,685,210 new cases of cancer will be detected in 2016 in the U.S alone. The most common ones are breast cancer, prostate cancer, colon and rectum cancer, lung and bronchus cancer, bladder cancer, melanoma, kidney and renal pelvis cancer, leukemia, and pancreatic cancer. Of these colorectal cancer is the third most common type of cancer in the world. This cancer is a result of uninhibited cell progression that occurs in the appendix, colon, and the rectum region. The common symptoms of colorectal cancer are bleeding in the stool, weight loss, fatigue, and irregular bowel movements. According to the World Cancer Research Fund International, approximately 1.5 million new cases of colorectal cancer are detected each year. Many clinical trials are being conducted to discover novel methods to treat colorectal cancer through fibroblast activation protein (FAP) inhibitors.

The increasing worldwide prevalence of various cancers, including breast cancer, colorectal cancer, prostate cancer, skin cancer, blood cancer, gastrointestinal tract cancer, and lung cancer, is the prime factor heightening the demand for anti-cancer drugs. In addition to this, the improvement of advanced therapeutic approaches, such as targeted therapies, immunotherapy, radiotherapy, and chemotherapy has significantly benefited the anti-cancer drugs market in recent years. Although not much progress has been made in fibroblast activation protein (FAP) inhibitors discovery for treating various cancer, this field possesses huge research and development opportunities in the near future.

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